WO2010011834A3 - Sunitinib et ses sels et leurs polymorphes - Google Patents

Sunitinib et ses sels et leurs polymorphes Download PDF

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Publication number
WO2010011834A3
WO2010011834A3 PCT/US2009/051530 US2009051530W WO2010011834A3 WO 2010011834 A3 WO2010011834 A3 WO 2010011834A3 US 2009051530 W US2009051530 W US 2009051530W WO 2010011834 A3 WO2010011834 A3 WO 2010011834A3
Authority
WO
WIPO (PCT)
Prior art keywords
sunitinib
polymorphs
preparation
acetate
malate via
Prior art date
Application number
PCT/US2009/051530
Other languages
English (en)
Other versions
WO2010011834A2 (fr
Inventor
Alexandr Jegorov
Ales Gavenda
Pavel Vraspir
Augusto Canavesi
Francesca Scarpitta
Original Assignee
Teva Pharmaceutical Industries Ltd.
Teva Pharmaceuticals Usa, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Teva Pharmaceutical Industries Ltd., Teva Pharmaceuticals Usa, Inc. filed Critical Teva Pharmaceutical Industries Ltd.
Priority to CA2731605A priority Critical patent/CA2731605A1/fr
Priority to US13/055,609 priority patent/US8618309B2/en
Priority to EP09790764A priority patent/EP2373642A2/fr
Priority to CN2009801381205A priority patent/CN102239163A/zh
Publication of WO2010011834A2 publication Critical patent/WO2010011834A2/fr
Publication of WO2010011834A3 publication Critical patent/WO2010011834A3/fr
Priority to IL210725A priority patent/IL210725A0/en
Priority to US13/944,699 priority patent/US9067915B2/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La présente invention concerne la préparation et la description de polymorphes de l'acétate de sunitinib et de la base de sunitinib et de la forme 1 du malate de sunitinib.
PCT/US2009/051530 2008-07-24 2009-07-23 Sunitinib et ses sels et leurs polymorphes WO2010011834A2 (fr)

Priority Applications (6)

Application Number Priority Date Filing Date Title
CA2731605A CA2731605A1 (fr) 2008-07-24 2009-07-23 Sunitinib et ses sels et leurs polymorphes
US13/055,609 US8618309B2 (en) 2008-07-24 2009-07-23 Sunitinib and salts thereof and their polymorphs
EP09790764A EP2373642A2 (fr) 2008-07-24 2009-07-23 Sunitinib et ses sels et leurs polymorphes
CN2009801381205A CN102239163A (zh) 2008-07-24 2009-07-23 通过乙酸舒尼替尼和它们的多晶型物制备苹果酸舒尼替尼的方法
IL210725A IL210725A0 (en) 2008-07-24 2011-01-18 Process for the preparation of sunitinib malate via sunitinib acetate and their polymorphs
US13/944,699 US9067915B2 (en) 2008-07-24 2013-07-17 Sunitinib and salts thereof and their polymorphs

Applications Claiming Priority (26)

Application Number Priority Date Filing Date Title
US13700508P 2008-07-24 2008-07-24
US61/137,005 2008-07-24
US8658908P 2008-08-06 2008-08-06
US61/086,589 2008-08-06
US8785908P 2008-08-11 2008-08-11
US61/087,859 2008-08-11
US8899808P 2008-08-14 2008-08-14
US8896108P 2008-08-14 2008-08-14
US61/088,998 2008-08-14
US61/088,961 2008-08-14
US9434108P 2008-09-04 2008-09-04
US61/094,341 2008-09-04
US9759208P 2008-09-17 2008-09-17
US61/097,592 2008-09-17
US10515408P 2008-10-14 2008-10-14
US61/105,154 2008-10-14
US10807808P 2008-10-24 2008-10-24
US61/108,078 2008-10-24
US11304408P 2008-11-10 2008-11-10
US61/113,044 2008-11-10
US14138508P 2008-12-30 2008-12-30
US61/141,385 2008-12-30
US16454209P 2009-03-30 2009-03-30
US61/164,542 2009-03-30
US17771709P 2009-05-13 2009-05-13
US61/177,717 2009-05-13

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US13/055,609 A-371-Of-International US8618309B2 (en) 2008-07-24 2009-07-23 Sunitinib and salts thereof and their polymorphs
US13/944,699 Division US9067915B2 (en) 2008-07-24 2013-07-17 Sunitinib and salts thereof and their polymorphs

Publications (2)

Publication Number Publication Date
WO2010011834A2 WO2010011834A2 (fr) 2010-01-28
WO2010011834A3 true WO2010011834A3 (fr) 2010-05-20

Family

ID=41110747

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2009/051530 WO2010011834A2 (fr) 2008-07-24 2009-07-23 Sunitinib et ses sels et leurs polymorphes

Country Status (5)

Country Link
US (2) US8618309B2 (fr)
EP (1) EP2373642A2 (fr)
KR (1) KR20110036588A (fr)
CA (1) CA2731605A1 (fr)
WO (1) WO2010011834A2 (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010041134A1 (fr) * 2008-10-10 2010-04-15 Medichem, S.A. Procédé pour la préparation d'un sel de malate de 2-indolinone substituée par pyrrole en position 3
WO2011058521A2 (fr) * 2009-11-12 2011-05-19 Ranbaxy Laboratories Limited Procédé de préparation de la forme cristalline i du sel d'acide l-malique de sunitinib
AU2011210327A1 (en) * 2010-01-29 2012-08-23 Ranbaxy Laboratories Limited Crystalline forms of L-malic acid salt of sunitinib
WO2011100325A2 (fr) 2010-02-09 2011-08-18 Sicor Inc. Polymorphes de sels de sunitinib
EP2542550A1 (fr) * 2010-03-04 2013-01-09 Ranbaxy Laboratories Limited Procédé de préparation directe de sel d'acide malique de sunitinib
CN104114550A (zh) 2012-03-23 2014-10-22 劳拉斯实验室私人有限公司 制备舒尼替尼及其酸加成盐的改进的方法
WO2014167436A2 (fr) * 2013-04-10 2014-10-16 Shilpa Medicare Limited Sel glucuronate de sunitinib et procédé pour sa préparation
ES2813877T3 (es) 2013-08-28 2021-03-25 Crown Bioscience Inc Taicang Distintivos de expresión génica predictivos de la respuesta de un sujeto a un inhibidor multicinasa y métodos de uso de los mismos
US9604968B2 (en) 2013-10-18 2017-03-28 Sun Pharmaceutical Industries Limited Pure crystalline Form II of L-malic acid salt of sunitinib and processes for its preparation

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030069298A1 (en) * 2001-08-15 2003-04-10 Pharmacia & Upjohn Company Crystals including a malic acid salt of a 3-pyrrole substituted 2-indolinone, and compositions thereof
WO2004075775A2 (fr) * 2003-02-24 2004-09-10 Sugen, Inc. Traitement d'une osteolyise excessive au moyen de composes d'indolinone
WO2009067674A2 (fr) * 2007-11-21 2009-05-28 Teva Pharmaceutical Industries Ltd. Polymorphes de base de sunitinib et procédés pour les préparer

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2290117T3 (es) 2000-02-15 2008-02-16 Sugen, Inc. Inhibidores de proteina quinasa 2-indolina sustituida con pirrol.
AR042586A1 (es) 2001-02-15 2005-06-29 Sugen Inc 3-(4-amidopirrol-2-ilmetiliden)-2-indolinona como inhibidores de la protein quinasa; sus composiciones farmaceuticas; un metodo para la modulacion de la actividad catalitica de la proteinquinasa; un metodo para tratar o prevenir una afeccion relacionada con la proteinquinasa
US6642232B2 (en) * 2001-10-10 2003-11-04 Sugen, Inc. 3-[4-Substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2- indolinone derivatives as kinase inhibitors
AU2003216282A1 (en) * 2002-02-15 2003-09-09 Pharmacia And Upjohn Company Llc Process for preparing indolinone derivatives
HN2003000272A (es) 2002-09-10 2008-07-29 Pharmacia Italia Spa Formulaciones que comprenden un compuesto de indolinona
KR101030720B1 (ko) * 2003-04-18 2011-04-26 후지필름 가부시키가이샤 표시장치용 차광막, 그 제조방법 및 이것을 형성하기 위한 조성물
EP1686987A4 (fr) 2003-11-26 2009-02-25 Scripps Research Inst Inhibiteurs ameliores a base d'indolinone de la proteine kinase
US20060009510A1 (en) * 2004-07-09 2006-01-12 Pharmacia & Upjohn Company Llc Method of synthesizing indolinone compounds
US20080193448A1 (en) 2005-05-12 2008-08-14 Pfizer Inc. Combinations and Methods of Using an Indolinone Compound
CA2715657A1 (fr) 2008-02-21 2009-08-27 Generics (Uk) Limited Nouveaux polymorphes et procedes de preparation
EP2280960A1 (fr) 2008-04-16 2011-02-09 Natco Pharma Limited Nouvelles formes polymorphes du sunitinib base
EP2315764A2 (fr) 2008-08-25 2011-05-04 Generics [UK] Limited Nouvelle forme cristalline et ses procédés de préparation
CN102197034A (zh) 2008-08-25 2011-09-21 基因里克斯(英国)有限公司 舒尼替尼的新型多晶型物及其制备方法
WO2010041134A1 (fr) 2008-10-10 2010-04-15 Medichem, S.A. Procédé pour la préparation d'un sel de malate de 2-indolinone substituée par pyrrole en position 3
EP2477978A1 (fr) 2009-09-16 2012-07-25 Ranbaxy Laboratories Limited Sels de sunitinib

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030069298A1 (en) * 2001-08-15 2003-04-10 Pharmacia & Upjohn Company Crystals including a malic acid salt of a 3-pyrrole substituted 2-indolinone, and compositions thereof
WO2004075775A2 (fr) * 2003-02-24 2004-09-10 Sugen, Inc. Traitement d'une osteolyise excessive au moyen de composes d'indolinone
WO2009067674A2 (fr) * 2007-11-21 2009-05-28 Teva Pharmaceutical Industries Ltd. Polymorphes de base de sunitinib et procédés pour les préparer
WO2009067686A2 (fr) * 2007-11-21 2009-05-28 Teva Pharmaceutical Industries Ltd. Hémi-l-malate de sunitinib, polymorphes et leur préparation, polymorphes de malate de sunitinib racémique, compositions contenant une base de sunitinib et de l'acide malique et leur préparation

Also Published As

Publication number Publication date
US9067915B2 (en) 2015-06-30
US20110118477A1 (en) 2011-05-19
KR20110036588A (ko) 2011-04-07
EP2373642A2 (fr) 2011-10-12
US20130296575A1 (en) 2013-11-07
WO2010011834A2 (fr) 2010-01-28
CA2731605A1 (fr) 2010-01-28
US8618309B2 (en) 2013-12-31

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